公开(公告)号：WO2015011119A2

公开(公告)日：2015-01-29

申请号：PCT/EP2014065674

申请日：2014-07-22

Applicant: BASF SE

Inventor： HAFNER ANDREAS ,  BLATTER FRITZ ,  SZELAGIEWICZ MARTIN ,  SIEBENHAAR BERND ,  CHIODO TIZIANA ,  HINTERMANN TOBIAS ,  SALVADOR BEATE ,  VOSSEN MARCUS

IPC: C07D417/12

CPC classification number: C07D417/12 ,  C07C55/12 ,  C07D213/80 ,  C07D275/06

Abstract: The present invention primarily relates to salts of Dasatinib, wherein the salts are in amorphous form. The salts described herein preferably comprise a cation of a compound of formula 1 and an anion of a second compound selected from the group consisting of glutaric acid, nicotinic acid and saccharin. The invention is further related to pharmaceutical compositions comprising such a salt. Furthermore, the invention relates to processes for preparing said salts. The invention also relates to several aspects of using said salt or pharmaceutical composition to treat a disease.

Abstract translation: 本发明主要涉及达沙替尼的盐，其中盐为无定形形式。 本文所述的盐优选包含式1化合物的阳离子和选自戊二酸，烟酸和糖精的第二化合物的阴离子。 本发明还涉及包含这种盐的药物组合物。 此外，本发明涉及制备所述盐的方法。 本发明还涉及使用所述盐或药物组合物治疗疾病的几个方面。

公开(公告)号：WO2013186726A3

公开(公告)日：2014-02-20

申请号：PCT/IB2013054832

申请日：2013-06-13

Applicant: BASF SE ,  BASF SCHWEIZ AG ,  BASF CHINA CO LTD

Inventor： CHIODO TIZIANA ,  HAFNER ANDREAS ,  HINTERMANN TOBIAS ,  SALVADOR BEATE ,  SZELAGIEWICZ MARTIN ,  BLATTER FRITZ ,  SIEBENHAAR BERND ,  VOSSEN MARCUS

IPC: C07D417/12 ,  A61K31/506 ,  A61P35/00

CPC classification number: C07D417/12 ,  A61K31/506 ,  C07B2200/07 ,  C07B2200/13 ,  C07C35/12 ,  C07C47/58 ,  C07C65/03 ,  C07C69/84 ,  C07D213/82 ,  C07D309/40 ,  A61K2300/00

Abstract: Provided are a multicomponent crystalline system (co-crystal), use thereof, as well as a process for obtaining the same. The said multicomponent crystalline system (co-crystal) comprises Dasatinib and a second compound selected from methyM-hydrobenzoate, nicotinamide, ethyl gallate, methyl gallate, propyl gallate, ethyl maltol, vanillin, menthol, or (lR,2S,5R)-(-)- menthol.

Abstract translation: 提供多组分结晶体（共晶体）及其用途，以及获得该组合物的方法。 所述多组分晶体系统（共晶体）包含达沙替尼和选自甲基 - 羟基苯甲酸甲酯，烟酰胺，没食子酸乙酯，没食子酸甲酯，没食子酸丙酯，乙基麦芽酚，香草醛，薄荷醇或（1R，2S，5R） - （ - ） - 薄荷脑

公开(公告)号：WO2015011120A3

公开(公告)日：2015-04-16

申请号：PCT/EP2014065675

申请日：2014-07-22

Applicant: BASF SE

Inventor： HAFNER ANDREAS ,  BLATTER FRITZ ,  SZELAGIEWICZ MARTIN ,  SIEBENHAAR BERND ,  CHIODO TIZIANA ,  HINTERMANN TOBIAS ,  SALVADOR BEATE ,  VOSSEN MARCUS

IPC: C07D417/12 ,  A61K31/506

CPC classification number: C07D417/12 ,  C07B2200/13 ,  C07D275/06

Abstract: The present invention primarily relates to molecular crystalline substances, preferably salts of Dasatinib in crystalline form, comprising a compound of formula 1, preferably a cation of a compound of formula 1, and a second compound selected from the group consisting of glutaric acid, nicotinic acid and saccharin, preferably an anion thereof. The invention is further related to pharmaceutical compositions comprising such a substance. Furthermore, the invention relates to processes for preparing said substances. The invention also relates to several aspects of using said substances or pharmaceutical compositions to treat a disease.

Abstract translation: 本发明主要涉及分子结晶物质，优选结晶形式的达沙替尼盐，其包含式1化合物，优选式1化合物的阳离子和选自戊二酸，烟酸 和糖精，优选其阴离子。 本发明还涉及包含这种物质的药物组合物。 此外，本发明涉及制备所述物质的方法。 本发明还涉及使用所述物质或药物组合物治疗疾病的若干方面。

公开(公告)号：EP2861589A4

公开(公告)日：2016-03-02

申请号：EP13804937

申请日：2013-06-13

Applicant: BASF SE

Inventor： CHIODO TIZIANA ,  HAFNER ANDREAS ,  HINTERMANN TOBIAS ,  SALVADOR BEATE ,  SZELAGIEWICZ MARTIN ,  BLATTER FRITZ ,  SIEBENHAAR BERND ,  VOSSEN MARCUS

IPC: C07D417/12 ,  A61K31/506 ,  A61P35/02

CPC classification number: C07D417/12 ,  A61K31/506 ,  C07B2200/07 ,  C07B2200/13 ,  C07C35/12 ,  C07C47/58 ,  C07C65/03 ,  C07C69/84 ,  C07D213/82 ,  C07D309/40 ,  A61K2300/00

公开(公告)号：ES2637829T3

公开(公告)日：2017-10-17

申请号：ES13804937

申请日：2013-06-13

Applicant: BASF SE

Inventor： CHIODO TIZIANA ,  HAFNER ANDREAS ,  HINTERMANN TOBIAS ,  SALVADOR BEATE ,  SZELAGIEWICZ MARTIN ,  BLATTER FRITZ ,  SIEBENHAAR BERND ,  VOSSEN MARCUS

IPC: C07D417/12 ,  A61K31/506 ,  A61P35/02

Abstract: Un sistema cristalino multicomponente (cocristal) que comprende un compuesto de fórmula 1 (INN: Dasatinib) **(Ver fórmula)** y un segundo compuesto seleccionado de metil-4-hidroxibenzoato, o nicotinamida, o galato de etilo, o galato de metilo, o galato de propilo, o etil maltol, o vanillina, o mentol, o (1R,2S,5R)-(-)-mentol.

公开(公告)号：AU2014295144B2

公开(公告)日：2017-06-15

申请号：AU2014295144

申请日：2014-07-22

Applicant: BASF SE

Inventor： HAFNER ANDREAS ,  BLATTER FRITZ ,  SZELAGIEWICZ MARTIN ,  SIEBENHAAR BERND ,  CHIODO TIZIANA ,  HINTERMANN TOBIAS ,  SALVADOR BEATE ,  VOSSEN MARCUS

IPC: C07D417/12 ,  A61K31/506

Abstract: The present invention primarily relates to molecular crystalline substances, preferably salts of Dasatinib in crystalline form, comprising a compound of formula 1, preferably a cation of a compound of formula 1, and a second compound selected from the group consisting of glutaric acid, nicotinic acid and saccharin, preferably an anion thereof. The invention is further related to pharmaceutical compositions comprising such a substance. Furthermore, the invention relates to processes for preparing said substances. The invention also relates to several aspects of using said substances or pharmaceutical compositions to treat a disease.

公开(公告)号：MX2016001096A

公开(公告)日：2016-04-25

申请号：MX2016001096

申请日：2014-07-22

Applicant: BASF SE

Inventor： SZELAGIEWICZ MARTIN ,  BLATTER FRITZ ,  CHIODO TIZIANA ,  HAFNER ANDREAS ,  HINTERMANN TOBIAS ,  SALVADOR BEATE ,  SIEBENHAAR BERND ,  VOSSEN MARCUS

IPC: C07D417/12

Abstract: La presente invención principalmente se refiere a sales de Dasatinib, en donde las sales están en forma amorfa. Las sales descritas en este documento comprenden un catión de un compuesto de fórmula 1 (ver Fórmula) y un anión de un segundo compuesto seleccionado del grupo que consiste en ácido glutárico, ácido nicotínico y sacarina. La invención se refiere en forma adicional a composiciones farmacéuticas que comprenden dicha sal. Además, la invención se refiere a procesos para preparar dichas sales. La invención se refiere a varios aspectos del uso de dicha sal o composición farmacéutica para tratar una enfermedad.

公开(公告)号：MX2016001095A

公开(公告)日：2016-04-25

申请号：MX2016001095

申请日：2014-07-22

Applicant: BASF SE

Inventor： SZELAGIEWICZ MARTIN ,  BLATTER FRITZ ,  CHIODO TIZIANA ,  HAFNER ANDREAS ,  HINTERMANN TOBIAS ,  SALVADOR BEATE ,  SIEBENHAAR BERND ,  VOSSEN MARCUS

IPC: C07D417/12 ,  A61K31/506

Abstract: La presente invención principalmente se refiere a sustancias cristalinas moleculares, preferentemente sales de Dasatinib en forma cristalina, que comprenden un compuesto de fórmula 1, preferentemente un catión de un compuesto de fórmula 1. (ver Fórmula) y un segundo compuesto seleccionado del grupo que consiste en ácido glutárico, ácido nicotínico y sacarina, un anión, preferentemente de los anteriores. La invención se refiere en forma adicional a composiciones farmacéuticas que comprenden dicha sustancia. Además, la invención se refiere a procesos para preparar dichas sustancias. La invención se refiere a varios aspectos del uso de dichas sustancias o composiciones farmacéuticas para tratar una enfermedad.

公开(公告)号：CA2917209A1

公开(公告)日：2015-01-29

申请号：CA2917209

申请日：2014-07-22

Applicant: BASF SE

Inventor： HAFNER ANDREAS ,  BLATTER FRITZ ,  SZELAGIEWICZ MARTIN ,  SIEBENHAAR BERND ,  CHIODO TIZIANA ,  HINTERMANN TOBIAS ,  SALVADOR BEATE ,  VOSSEN MARCUS

IPC: C07D417/12

Abstract: The present invention primarily relates to salts of Dasatinib, wherein the salts are in amorphous form. The salts described herein preferably comprise a cation of a compound of formula 1 and an anion of a second compound selected from the group consisting of glutaric acid, nicotinic acid and saccharin. The invention is further related to pharmaceutical compositions comprising such a salt. Furthermore, the invention relates to processes for preparing said salts. The invention also relates to several aspects of using said salt or pharmaceutical composition to treat a disease.

公开(公告)号：CA2832343A1

公开(公告)日：2012-10-26

申请号：CA2832343

申请日：2012-04-16

Applicant: BASF SE

Inventor： HAFNER ANDREAS ,  BLATTER FRITZ ,  SZELAGIEWICZ MARTIN ,  SIEBENHAAR BERND

IPC: C07D239/42 ,  A61K31/505 ,  A61P9/00

Abstract: A novel solid form of Rosuvastatin comprises as the active ingredient a salt of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)-amino]pyrimidin-5-yl]-(3R,5S)-3,5-dihydroxyhept-6-enoic acid] and vanillin or vanillin derivatives. The crystal comprising the two components, and minor amounts of water, shows improved properties such as crystallization behavior stability and decreased hydroscopic behavior.